Compound having activity of blocking NMDA receptor channel, and pharmaceutical agent using the same

Abstract

[PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.

What is claimed is: 
     
       1. A pharmaceutical formulation comprising a) a compound represented by the following formula (1), a salt thereof, or a hydrate of the compound or the salt, 
       
         
           
           
               
               
           
         
       
       wherein the B-ring, condensed to the A-ring and the C-ring, is azepine, R 1 -R 5  are each independently formyl, acyl, hydrogen, alkyl, alkoxy, halogen, hydroxy, amino, aryl or carboxamido, and at least either of R 1  or R 2  is one carboxamide group having a polyamine structure containing three or more amino groups, wherein an amino group of any carboxamido group is excluded, and R 1 -R 5  are identical or different, and b) a pharmaceutically acceptable carrier. 
     
     
       2. A pharmaceutical formulation comprising a) a compound is represented by formula (4), a salt thereof, or a hydrate of the compound or the salt, 
       
         
           
           
               
               
           
         
       
       and b) a pharmaceutically acceptable carrier. 
     
     
       3. A compound represented by the following formula (1), or a pharmaceutically acceptable salt thereof, 
       
         
           
           
               
               
           
         
       
       wherein the B-ring, condensed to the A-ring and the C-ring, is azepine, R 1 -R 5  are each independently formyl, acyl, hydrogen, alkyl, alkoxy, halogen, hydroxy, amino, aryl or carboxamido, and at least either of R 1  or R 2  is one carboxamide group having a polyamine structure containing three or more amino groups, wherein an amino group of any carboxamido group is excluded, and R 1 -R 5  are identical or different. 
     
     
       4. A compound represented by formula (4), 
       
         
           
           
               
               
           
         
       
     
     
       5. A compound represented by the following formula (1), a salt thereof, or a hydrate of the compound or the salt, 
       
         
           
           
               
               
           
         
       
       wherein the B-ring, condensed to the A-ring and the C-ring, is azepine, R 1 -R 5  are each independently formyl, acyl, hydrogen, alkyl, alkoxy, halogen, hydroxy, amino, aryl or carboxamido, and at least either of R 1  or R 2  consists of a single carboxamide group and a polyamine structure containing three or more amino groups, wherein an amino group of any carboxamido group is excluded, and R 1 -R 5  are identical or different and wherein said polyamine structure is directly bonded to said single carboxamide group. 
     
     
       6. The pharmaceutical formulation of  claim 1 , wherein the polyamine structure is a non-aromatic polyamine structure. 
     
     
       7. The compound of  claim 5 , wherein the polyamine structure is a non-aromatic polyamine structure.